产品
编 号:F386743
分子式:C20H25ClN2OS
分子量:376.94
产品类型
结构图
CAS No: 54-84-2
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产品详情
生物活性:
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
体内研究:
Cinanserin (5 mg/kg; intravenous injection; for 2 hours; male Wistar rats) treatment significantly reduces systemic burn edema to shamburn levels. Leukocyte-endothelial interactions are significantly reduced by administration of Cinanserin.Animal Model:Male Wistar rats (250 g) underwent thermal injury
Dosage:5 mg/kg
Administration:Intravenous injection; for 2 hours
Result:Significantly reduced systemic burn edema to shamburn levels..
体外研究:
Cinanserin/Cinanserin hydrochloride have binding affinity to SARS-CoV 3CLpro, HCoV-229E 3CLpro, with the KD values of 49.4 μM/78.0 μM for SARS-associated coronavirus (SARS-CoV) 3CLpro and 18.2 μM/36.6 μM for human coronavirus 229E (HCoV-229E) 3CLpro.The IC50 values of Cinanserin and Cinanserin hydrochloride for inhibiting the catalytic activity of SARS-CoV 3CLpro are calculated as 4.92 μM and 5.05 μM, respectively, The corresponding IC50 values for HCoV-229E 3CLpro are 4.68 μM and 5.68 μM. None of the compounds have inhibitory activity against HRV-14 3Cpro at concentrations up to 200 μM.